Quinoxaline derivatives as antiparasitic drugs: proof of concept

• Grant number: 16/13894-8
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• Start date: September 01, 2016
• End date: February 28, 2017
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Agreement: GlaxoSmithKline
• Principal Investigator: Arlene Gonçalves Corrêa
• Grantee: Valéria Aquilino Barbosa
• Host Institution: Centro de Ciências Exatas e de Tecnologia (CCET). Universidade Federal de São Carlos (UFSCAR). São Carlos , SP, Brazil
• Company: Universidade Federal de São Carlos (UFSCAR). Centro de Ciências Exatas e de Tecnologia (CCET)
• Associated research grant: 13/50680-8 - Quinoxaline derivatives as antiparasitic drugs: proof of concept, AP.PITE

Abstract

Quinoxalines are a class of heterocyclic compounds that have been intensively studied for their biological activities, showing promising activity against protozoa. In an ongoing study towards the discovery of new antiparasitic compounds, we have synthesized a library of quinoxaline derivatives, which has been evaluated in vitro against epimastigote, promastigote, and trypomastigote forms of Trypanossoma cruzi and intracellular amastigote and promastigote forms of Leishmania amazonensis. From this screening, we have selected the most active compounds for in vivo and mechanistic studies. The main objective of this project is to prove the biological activity of these compounds in the drug development for tropical diseases such as Chagas'disease and leishmaniasis. More specifically, our goal is the synthesis of quinoxaline derivatives aiming at improving yield, a scalable and safe process and decreasing of chemical residues. Looking into pharmaceutical application of these drug candidates, they will be evaluated in vitro and in vivo in order to determine their mechanism of action against T. cruzi and L. amazonensis. (AU)